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Cholesterylchitosan nano carrier as well as medicament-carried nano particle and preparation method thereof

A technology of chitosan and nanocarriers, which is applied in the field of selective cholesteric chitosan nanocarriers and its drug-loaded nanoparticles and manufacturing, to achieve improved solubility, high drug-loading capacity, and good biocompatibility Effect

Inactive Publication Date: 2010-10-06
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the selective cholesterylation of chitosan and the preparation of chitosan derivative nanoparticles as drug carriers have not been reported.

Method used

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  • Cholesterylchitosan nano carrier as well as medicament-carried nano particle and preparation method thereof
  • Cholesterylchitosan nano carrier as well as medicament-carried nano particle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Embodiment 1: the preparation of selective cholesteric chitosan

[0023] Its synthetic route is:

[0024]

[0025] Dissolve 2g of cholesterol and 1.6g of succinic anhydride in 12mL of pyridine, stir and react at 40-50°C for 72h, the reaction solution is precipitated in glacial hydrochloric acid solution, filtered, the precipitate is washed with distilled water until neutral, and recrystallized in ethyl acetate / ethanol system , and dried to obtain cholesteryl succinate (CHS); weigh 0.5 g of chitosan and 1.33 g of phthalic anhydride and disperse them in 10 mL of DMF (water content 5%, mL / mL), and react at 120° C. for 8 h under nitrogen protection. Pour the reaction solution into ice water, filter, wash the precipitate with methanol, and dry under vacuum at 45°C to obtain phthalylated chitosan (PHCS); weigh 0.5g of CHS, 1.12g of PHCS and a certain amount of EDC·HCl and NHS Dissolve in 50mL DMF, stir and react at room temperature for 72h, filter, wash and purify the pro...

Embodiment 2

[0027] Embodiment 2: Preparation of selective cholesteric chitosan drug-loaded nanoparticles

[0028] Weigh 20mg of O-CHCS and dissolve in 0.1mol / L acetic acid solution, transfer the solution into a dialysis bag, and dialyze in normal saline for 24h (change the water every 1h for the first 3h, then every 3h thereafter), constant volume, and use 0.45 The O-CHCS blank nanoparticles were obtained by filtering with a μm filter membrane; 0.8 mL of all-trans retinoic acid (ATRA) dimethyl sulfoxide solution (5 mg / mL) was added to the blank nanoparticle solution under ultrasonication in an ice-water bath, and the probe was ultrasonicated in an ice-water bath Treat 3 times (2min each time, output power 50W, pulse width 2s, intermittent time 2s), dialyze the solution in normal saline or distilled water for 9h (change the water every 1h for the first 3h, then change every 3h thereafter), constant volume , to obtain O-CHCS drug-loaded nanoparticles.

[0029] The prepared selective choles...

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Abstract

The invention relates to a selective cholesteryl chitosan nano particle and a preparation method thereof. The preparation method comprises the following steps of: preparing cholesteryl succinate (CHS) and phthaloyl chitosan (PHCS) by using cholesterol, succinic anhydride, phthalic anhydride and chitosan as raw materials and then reacting the CHS and the PHCS to prepare the cholesteryl chitosan nano particle, wherein the particle size is 100-200 nm, the molar ratio of the cholesterol to the succinic anhydride is 1-30:3-90, and the molar ratio of the chitosan to the phthalic anhydride is 1-60:3-180. An amphiphilic polymer obtained with the preparation method comprises a hydrophilic polysaccharide skeleton and a hydrophobic cholesterol branched chain and can automatically gather in a water medium to form the nano particle with a nucleus-shell type structure; and the nano particle has positive charge, is beneficial to the entrapment of hydrophobic medicaments, albumen and DNA, and has the advantages of simple preparation method, good repeatability, easy industrial production, high medicament-carrying efficiency and favorable slow-releasing effect.

Description

Technical field: [0001] The invention relates to a selective cholesteric chitosan nano-carrier, drug-loaded nano-particles and a manufacturing method thereof. Background technique: [0002] As a new type of drug delivery and controlled release carrier, biodegradable polymer nanoparticles, especially those based on polysaccharides, have good biocompatibility, ultra-fine size, reasonable in vivo distribution and efficient drug utilization. rate has received increasing attention in recent years. Biodegradable polymer nanoparticles can not only enhance the stability of drugs, improve curative effect, and reduce side effects, but also can be enriched in tumor lesions due to the EPR effect (Enhanced Permeability and Retention Effect), realizing the "passive targeting of tumor tissue". ", is an ideal carrier for embedding anticancer drugs, peptides, proteins, nucleic acids, vaccines and genes. [0003] Chitosan (chitosan, CS) is a class of positively charged linear copolymers con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36C08B37/08A61P35/00
Inventor 张其清陈名懋李学敏刘玲蓉杨文智刘刘
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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